Oil from Momordica charantia L., its method of preparation and uses

ABSTRACT

The present invention relates to a novel oil extracted from the seeds of  Momordica charantia  L., for topical application to a body of mammal and used as anti-inflammatory, anti-arthritic, vasculodilatory and wound healing agent, said oil essentially comprising capric acid 0.7–1.2% by wt., lauric acid 0.6–1% by wt., palmitic acid 42–5.0% by wt., stearic acid 59–62% by wt., oleic acid 13–15% by wt., archid acid 3–5% by wt., linoleic acid 8–10% by wt., and other undetected minor acids 6–8% by wt.; and a process for producing such oil.

FIELD OF THE INVENTION

The invention relates in general, to a novel oil extracted from theseeds of Momordica charantia L., (bitter gourd), its preparation and useas anti-inflammatory, anti-arthritic, vasculodilatory and wound healingagent.

BACKGROUND

The invention relates to a novel oil extracted from the seeds ofMomordica charantia L., (bitter gourd). Momordica charantia is aperennial herb of the family Cucurbitaceae, widely grown in Asia. Theherb is endemic to tropical countries like India, S. Africa,Philippines, China and Burma. The species of Momordica found in westerncountries are different from the tropical species in that, the plantsdiffer in morphological and organoleptic properties. Various parts ofthis plant, especially the fruits, have been widely used for preparationof hypoglycemic pharmaceutical compositions.

The extract/juice of the fruit is known to exhibit hypoglycemicproperties and often recommended to reduce the blood sugar levels inpatients suffering from diabetes mellitus.

DESCRIPTION OF RELATED PRIOR ART

Natural oils from various plant sources have been used in variety ofapplications. For instance, U.S. Pat. No. 5,916,573 discloses grapeseedoil for tropical application on the skin. Similarly, U.S. Pat. No.5,900,240 discloses herbal compositions and their use as hypoglycemicagents. The composition of this Patent comprises a mixture, of which theextract of Momordica charantia is one ingredient. This compositionattends only to hypoglycemic conditions.

Various pharmaceutical compositions employing extracts from Momordicacharantia are available in the market. However, most of thesecompositions are for oral administration and do not attend to theexternal manifestations and pathological conditions such asinflammations and wounds. Though, Momordica sp. has been the subject ofextensive study all over the world, there is no literature on oilextracted from Momordica charantia L. In fact, there is a dearth of oilexhibiting anti-inflammatory, vasculodilatory, anti-arthritic propertiesin the market. As such, there is no report in literature on oilextracted from Momordica charantia L. In other words, the presentinvention is the first detailed study on Momordica oil and itsproperties.

OBJECTS OF THE INVENTION

It is an object of the invention to provide oil extracted from the seedsof Momordica charantia L. and a composition prepared therefrom.

Another object of the invention is to provide a method for theextraction of oil from the seeds Momordica charantia L.

Yet another object is to provide a method for the treatment ofinflammations, wounds, arthritis, neuropathy developed due to diabetesmellitus and vasculodilatory conditions in humans and animals.

Still another object of the invention is to provide an oil compositioncomprising the oil from Momordica charantia L. mixed with any suitablepharmaceutically acceptable additives/carriers.

SUMMARY OF THE INVENTION

In accordance with the above and other objectives, the inventionprovides an oil composition prepared from the oil extracted from theseeds of Momordica charantia L., essentially comprising a mixture ofCapric acid, Lauric acid, Palmitic acid, Stearic acid, Oleic acid,Archidic acid, Linoleic acid, other undetected minor acids and esters.

The invention also provides a process for the extraction of oil from theseeds of Momordica charantia L., using non-polar solvents.

Further, the invention teaches the use of the oily composition in thetreatment of arthritis, diabetes and other conditions developed indiabetic patients.

DETAILED DESCRIPTION OF THE INVENTION

Accordingly, the invention provides oil extracted from the seeds ofMomordica charantia L., essentially comprising:

1. Capric acid 0.7–1.2% 2. Lauric acid 0.6–1%   3. Palmitic acid4.2–5.0% 4. Stearic acid 59–62% 5. Oleic acid 13–15% 6. Archid acid 3–5%7. Linoleic acid  8–10% 8. Other undetected minor acids 6–8%Further, the invention provides a method for the extraction of oil fromthe seeds of Momordica charantia L., comprising the steps of:

-   -   (i) grinding the dry seeds to a fine powder in a suitable mill,    -   (ii) treating the pulverized seeds with a mixture of non-polar        solvents,    -   (iii) allowing the mixture to stand for 48 hours at room        temperature so that the oil separates out,    -   (iv) collecting the oil from the supernatant layer using a        separatory funnel,    -   (v) refluxing the mixture obtained in step (vi) with any        non-polar solvent to remove the last traces of oil, and    -   (vi) purification of the oil by precipitating the salts with        impurities in it.

In one embodiment, the seeds of Momordica charantia L., are split,washed thoroughly with water, 2–3 times to render it substantially freefrom impurities and dried under vacuum, before using the seeds forextraction of the oil.

In another embodiment, the non-polar solvents used for extraction of oilmay comprise a mixture of acetone with an aromatic or aliphatichydrocarbon selected from the group of benzene, hexane, petroleum etherand ethyl ether.

In yet another embodiment, the ratio of acetone to the aliphatic oraromatic hydrocarbon in the non-polar solvent mixture may be 2:1.

In yet another feature, 2–5% zinc acetate dissolved in water may be usedto precipitate the proteins and other impurities in the oil.

In another feature, the oil extracted is analyzed for its fatty acidcontents using gas liquid chromatography (GLC).

It may be noted that most of the plant parts of Momordica contain theoil disclosed by the invention, in varying degrees. As such, the oil maybe extracted using any plant parts preferably seeds.

A novel oil composition comprising oil extracted from the seeds ofMomordica charantia L 70 to 80% by wt., one or more vegetable oils—15 to25% by wt., fragrance oil —3% by wt, essential oil—1% by wt, and atleast one perfume component—2% by wt.

In accordance with the present invention, the oil obtained from theseeds of Momordica charantia L., is thick reddish-orange in colour,having bitter taste. The oil extracted by the method describedhereinabove is obtained in 98.5% purity. The oil is water immiscible.However, it is soluble in non-polar solvents like benzene, petroleumether, ethyl ether, acetone and hexane.

The applicant through continued usage and after rigorous experimentationhas found that the oil exhibits anti-inflammatory, anti-arthritic,vasulodilatory properties as it contains several unsaturated componentslike linoleic acid, oleic acid etc which are known for their antioxidant& anti-inflammatory properties.

It is found that the oil extracted from Momordica charantia L., is verythick and it is preferably used with diluents. Preferably, the oil maybe mixed with other essential or vegetable oils. The essential oils thatmay be mixed with the oil from Momordica charantia could be selectedfrom coconut oil, sesame oil, sunflower oil, olive oil, palm oil,groundnut oil or any such food grade oil. Further, it is found that whensuch food grade oils are mixed with the oils of Momordica, thepenetration of the oil mixture into the outermost layers of the skin isenhanced to a great extent. The Momordica oil composition of theinvention is prepared by mixing the 75% of the oil of Momordicacharantia L., with vegetable oils selected from coconut oil, sesame oilsunflower oil, palm oil, olive oil or groundnut oil.

Momordica charantia oil composition may be prepared by mixing the oilextracted from Momordica charantia L, with vegetable oils and essentialoils. The composition may also include, if desired, a botanicalfragrance oil such as lavender oil, sandalwood oil, rose oil andgeranium oils. The oil composition may further include a perfumecomponent or other pharmaceutically acceptable additives. The oilcomposition is generally in the form of oil, cream, lotion, gel,capsule, suspension, solutions, or emulsion or a combination thereof,though the formulation is not limited to these forms. The oilcomposition of the invention, the oil extracted from Momordica charantiais thoroughly mixed and stirred with the essential oils at roomtemperature for 12 hours. The remaining components such as fragranceoil, perfume component or other additions are then added to thecomposition and vortexed for 10 hours at room temperature. The oilcomposition is applied in an amount sufficient to cover the targetedarea of the clean, dry skin, with the fingertips or a cotton swab. Inregions where there is no external injury or wound, it is advisable tomassage the region locally for a 1–2 minutes after application of theoil composition. The penetrating effect of the oil composition to theoutermost layers of the skin may be further enhanced by the addition oflittle vitamin E or oil containing vitamin E.

Studies on the oil composition of the invention suggest that topical useof the oil composition is safe and effective. There are no side effects.

BRIEF DESCRIPTION OF THE ACCOMPANYING DRAWINGS

The accompanying drawings are photographs of the pathological conditionsof patients and the improvements therein:—

FIG. 1 represents the gangrenous wound on the sole of the right foot ofthe patient described in example No. 5, prior to the treatment.

FIG. 2 represents the condition of the sole after two months oftreatment with the oil composition of the invention.

FIG. 3 represents the gangrenous wound on the left foot of the malepatient in example No. 6 prior to the treatment.

FIG. 4 represents the condition of the wound on the same patient onemonth after application of the oil composition of the invention.

FIG. 5 represents the condition of the foot of the same patient twomonths after application of the oil composition of the invention.

The invention is described in detail with respect to the followingexamples which are provided as illustrative embodiments only. Theseexamples should not be construed to limit the scope of the invention inany manner. Modifications and alterations of the invention that may beapparent to those in the art are deemed to be included within the scopeof the invention.

EXAMPLE—1 Oil Preparative Example

Extraction of Oil from Momordica charantia L.:

100 gms of dry seeds were taken from the ripe fruits of Momordicacharantia L.,. The seeds were split. The split seeds were thenthoroughly washed with water 34 times to render them substantially freeof all impurities. The seeds were then dried under vacuum and pulverizedto a fine powder using a milling device. Any other conventional devicemay also be used. The fine powder was then treated with acetone hexanesolvent mixed in the ratio 1:2. The mixture was stirred thoroughly andallowed to stand for 48 hours at room temperature. The oil layer wasseparated. The oil that separates out as supernatant layer wascollected. The oil was then treated with 2–5% zinc acetate dissolved inwater so that the salts, last traces of proteins and other impuritiesare precipitated. The oil was centrifuged and analyzed on gas-liquidchromatograph. The oil purified using gas liquid chromatograph showedthe presence of the following fatty acids:

-   -   Capric acid 0.8%    -   Lauric acid 0.70%    -   Palmitic acid 4.8%    -   Stearic acid 60.3%    -   Oleic acid 13.0%    -   Archidic acid 3.0% and    -   Linoleic acid 10.0%        Other minor undetected components and acids 6.4%. The oil also        contains esters and other undetected minor ingredients.

EXAMPLE 2 Extraction of Oil from Momordica charantia L.

200 gms of dry seeds were taken from the ripe fruits of Momordicacharantia L.,. The seeds were split. The split seeds were thenthoroughly washed with water 3–4 times to render them substantially freeof all impurities. These seeds were then dried under vacuum andpulverized to a fine powder using a milling device.

Any other conventional devices may also be used. The fine powder wasthen treated with acetone benzene solvent mixed in the ratio 1:2. Themixture was stirred thoroughly and allowed to stand for 48 hours at roomtemperature. The oil in the supernatant layer was separated using aseparatory funnel. The filtrate was refluxed with acetone-benzene andthe process was repeated 2–3 times to separate out the last traces ofoil. The oil that separates out as supernatant layer was collected. Theoil was then treated with 2–5% zinc acetate dissolved in water so thatthe salts., last traces of proteins and other impurities areprecipitated. The oil was centrifuged and analyzed on gas-liquidchromatograph.

The oil purified using gas liquid chromatograph showed the presence ofthe following fatty acids:

-   -   Capric acid 0.9%    -   Lauric acid 0.70%    -   Palmitic acid 4.8%    -   Stearic acid 60.1%    -   Oleic acid 13.81%    -   Archidic acid 3.28% and    -   Linoleic acid 10.00%    -   Other minor undetected acids 6.11%.

The oil also contains esters and other undetected minor ingredients.

EXAMPLE 3 Preparation of Oil Composition

The oil extracted from Momordica charantia L., as discussed inpreparative examples 1–2 was kept in a beaker. Pure sesame oil was addedto it in the ratio 3:1. The mixture was stirred continuously andthoroughly for 4–10 hours. Thereafter, fragrance oil like sandalwood oilas well as a perfume component were added to the mixture and stirredcontinuously and thoroughly for 4–10 hours. The formulation thusprepared stored in a container in a cool dry place.

The oil composition of the present invention can be formulated in a widevariety physical forms which include solutions, lotions, creams, oils,gels, sticks, sprays, ointments, balms, pastes, aerosols etc.

For preparation of an ointment, the active ingredients of the oilcomposition can be incorporated in any pharmacologically acceptablecarrier, which is suitable for topical administration to the human skin.As such, the pharmacologically acceptable carrier must be of sufficientpurity and have low toxicity to render it suitable for administration toa human. The carrier may represent a major portion of the total portionof the composition from at least 80%.

The composition of the invention may be formulated as a cream using asuitable carrier system.

A formulation may be prepared by introducing the oil composition into alotion vehicle comprising glycerin, mineral oil, glycol stearate andother additives commonly known as Vasline Brand Intensive care lotion.

The following oil composition of the invention was prepared

-   -   Capric acid 0.9%    -   Lauric acid 0.8%    -   Palmitic acid 4.2%    -   Stearic acid 60.90%    -   Oleic acid 13.30%    -   Archidic acid 3.20% and    -   Linoleic acid 9.80%    -   Other minor undetected components and acids 6.90%        Creams, lotions, gels and other forms of the oil composition        were made and tested as illustrated in the following examples:        Case Histories:

The following are examples of a series of confirmed cases of patientssuffering from arthritis, diabetes, open wounds, inflammations etc.treated with the oil composition of the invention. Generally, themedication comprised tropical application of the oil composition (invarious forms such as gels, lotions, suspensions, creams, etc.). The agegroup of these patients ranged from 30–80 years. The average duration ofillness in the population was more than 5–6 years. All the patientsprior to the treatment with the composition of the invention were usingstandard causes of therapy, exercise etc. Upon commencement with the oilcomposition as disclosed herein, the patients refrained from using othermedications, except yoga and exercises. Specific excerpts from each casehistory is disclosed in the following examples.

EXAMPLE 4

A 30 year old Female working as a Receptionist had a bruise at her rightelbow The oil composition was applied to the bruise caused at the elbow.The elbow was first cleaned and dried and the oil composition wasapplied slowly using a cotton swab. The oil composition was regularlyapplied after every 4 hours, for about 3–5 weeks. At the end of 15 days,the bruise healed completely.

EXAMPLE 5

The subject was a 65 year old male. This patient had a gangrenous woundon his right foot. The gangrene was in its advanced stages. It was asevere case of gangrene affliction. As there was no fresh blood supply,no healing constituted veins. The oil formulation of the invention wasapplied by the patient for about 10–12 weeks topically. After eachapplication, the patient reported relief from the pain he suffered. Atthe end of the 6^(th) week itself, the wound started drying up andeventually after the 12 week the wound had healed completely. FIG. 1depicts the gangrenous wound at the time of commencement of thetreatment using the oil formulation of the invention. FIG. 2 shows thedried wound at the end of the 12^(th) week of the treatment.

EXAMPLE 6

A 45 year old female patient. This patient was chronic diabetic. She hada gangrenous wound on her left leg. The patient commenced application ofthe oil of the invention in the month of July 1997. After 1 month ofusage, the patient found great relief. The wound had started showingsigns of drying up and the patient also experienced relief from pain. Atthe end of 14 weeks itself, the wound had healed up completely anddried.

EXAMPLE 7

In one case, a 52 year old male had a leg ulcer, three to four inches indiameter. The ulceration was due to destruction of cellular componentsin the area. The patient was on standard medication. The patient cleanedthe wound and applied the oil composition to the affected area dailyevery 4 hours. The treatment continued for 4 months. At the end of thesecond month, the wound had stinted drying up and showed signs ofhealing. After the third month, the healing was far advanced. By the endof the fourth month, the wound had healed completely and the tissues hadcommenced regeneration.

EXAMPLE 8

The next case involves a 53 year old market researcher based in Delhi,India, having a wet gangrene of the second toe with neurotic nail bed.The subject was unable to walk and was in great pain. He commenced usageof the oil composition of the invention, applying it about 3 times aday. The treatment continued for 2 months at the end of which, the nail,its bed as well as the toe had healed completely. After the third month,the subject had a normal toe.

EXAMPLE 9

A 35 year old male. Chartered Accountant suffered from osteoarthritisfor more than 6 years. He complained of constant pain in the right kneeand was unable to walk without a cane. His movements were restricted asthe knee had become nearly stiff. Examination revealed that the synovialfluid had dried which lead to muscular tension. He had used oral drugsand pain killers, though of no avail.

This subject used the composition of the invention for about 3 monthsapplying it continuously on the knee 3–4 times a day. After the firstweek the pain had reduced to a great extent. The subject was advisedexercises to the extent possible. After 2 weeks, the patient could flexthe knee to 45° with no pain. After 6 weeks, he could flex and rotatethe knee in full range. He continued to apply the composition and after8 weeks, was able to walk freely.

EXAMPLE 10

In another case, a housewife aged 52 years suffered from obesity. Inaddition, the patient complained of pain in the knee and ankle due toinflammation. The patient could hardly walk. She was using standardmedication comprising drugs and injections, which did not help her much.

When the patient started using the composition of the invention,(application on the knee & ankle 4 times a day) she experienced reliefin the dumb constant pain in the first week itself. After 2–3 weeks, shecould stand and start walking to a limited extent. At the end of the3^(rd) week, upward and downward movement at the ankle was possible. Theknee was capable of flexing upto 45 degrees. After 8 weeks, the patientcommenced regular walking, full movement/rotation of the knees andankles.

EXAMPLE 11

A 32 year old female, working as a typist was suffering for more than ayear, from spondylitis. The patient was advised to apply the oilcomposition of the invention regularly 3–4 times a day with massaging ofthe afflicted area. The medication gave her relief from pain in the2^(nd) week itself. After 3–4 weeks, the patient could rescue neckmovements. Full movements were observed after 12 weeks.

EXAMPLE 12

In one case, a female Laboratory Assistant aged 42 years had developedvaricose vein. The native of her occupation required her to stand forlong hours and she had the habit of wearing high heeled shoes. As aresult, the leg muscles were stretched for long hours withoutrelaxation. The entire body weight concentrated on her joints andankles.

The stress caused capillaries to burst at the calf and blood thataccumulated in the leg could be seen as blue spots and thick veins.

The Patient was recommended exercise and was advised to massage the oilcomposition of the invention at least 4 times a day. After 3 weeks, itwas observed that the blue spots spread and after treatment for 10weeks, the spots disappeared.

EXAMPLE 13

A 48 years old woman, working as an administrator in a firm, complainedof osteoartritis. She had telescoping of the proximal interphalangealjoints of the left index finger. Minimal fusion was observed in thephalanges of both hands.

The patient was advised to apply the oil composition of the inventionabout 4 times a day, coupled with regular exercise. The patient reportedrelief from pain after 2 weeks, she reported restoration of function ofboth hands.

EXAMPLE 14

A manager aged 58 years, employed in a Bank, was suffering from diabetesmellitus. He also reported neuropathic symptoms with the rise in bloodlevel. This patient was advised to apply the oil composition of theinvention 4 times a day on his legs. He experienced relief and after 18weeks reported complete relief from these symptoms.

EXAMPLE 15

A dog aged 3 years was wounded in a dog fight. The dog had a grievouswound on its left foreleg. The wound was about 1 cm in diameter andabout ½ mm deep. The wound was cleaned and the oil composition of theinvention was applied to it regularly after every 4 hours. After 10 daysthe wound started drying up giving rise to regeneration of tissues atthe site of injury. After 30 days it was found that the wound hadcompletely healed.

EXAMPLE 16

A horse aged 4 years was injured by a nail at the stable. The wound was3 cm long and about ½ mm deep. This wound was cleaned thoroughly and theoil composition of the invention was applied to it nearly 3–4 times aday. After 10 days, sufficient amount of the tissue had grown over thewounded area and after 25 days, complete healing was observed.

The following is a table which gives the details of the patients treatedusing the oil composition of the invention:—

Sex of the Disease/pathol- S. patient No of ogical No. treated patientscondition General observations 1. Females 85 Gangrene The oilcomposition of the invention was applied for about 25 weeks for completehealing. 2. Male 125 Gangrene The oil composition of the invention wasapplied for about 20–30 weeks for complete healing. 3. Female 32Spondylitis The patients suffered spondylitis from the neck region andthe lumbar region. Upon application of the oil composition for about6–12 weeks, the patients experienced relief and could resume normalfunctions. 4. Male 65 Spondylitis The patients suffered from pain in theneck, lumbar and lower back. Oil composition of the invention wasapplied for 6–15 weeks for complete relief. 5. Female 63 RheumatoidPatients suffered from pain arthritis in the joints. Oil composition ofthe invention was applied for 6–10 weeks for complete relief. 6 Male 56Rheumatoid Patients suffered from pain arthritis in the joints. Oilcomposition of the invention was applied for 6–12 weeks for completerelief. 7 Female 45 Neurophathic Patients suffered from diabetesmuscular pain in the legs and hands. The oil composition was applied for15 weeks for complete relief. 8 Male 73 Neurophathic Patients sufferedfrom diabetes muscular pain in the legs and hands. The oil compositionwas applied for 15 weeks for complete relief.

1. Oil extracted from the seeds of Momordica charantia L., useful asanti-inflammatory, anti-arthritic, vasculodilatory and wound healingagent, said oil comprising essentially of: Capric acid 0.7+14 1.2% bywt. Lauric acid +11 +12 0.6+14 1% by wt. Palmitic acid 4.2+14 5.0% bywt. Stearic acid +12 +12 59+14 62% by wt. Oleic acid +12 +12 13+14 15%by wt. Archidic acid +10 +12 +12 3+14 5% by wt. Linoleic acid +11 +12+12 8+14 10% by wt. Other undetected minor acids +12 +12 +10 6+14 8% bywt.


2. Oil as claimed in claim 1, comprising: Capric acid 0.9% by wt. Lauricacid 0.8% by wt. Palmitic acid 4.2% by wt. Stearic acid 60.90% by wt.+10Oleic acid 13.30% by wt.+10 Archidic acid 3.20% by wt.+11 Linoleic acid9.80% by wt.+11 Other undetected minor acids 6.90% by wt.+11


3. A process for preparing the oil of claim 1, comprising the steps of:(i) grinding dry seeds to a fine powder in a suitable mill, (ii)treating the pulverized seeds with a mixture of non-polar solvents,(iii) allowing the mixture to stand for 48 hours at room temperature sothat the oil separates out, (iv) collecting the oil from the supernatantlayer using a separating funnel, (v) refluxing the mixture obtained instep (iv) with any non-polar solvent to remove the last traces of oil,(vi) purifying the oil by adding 2–5% zinc acetate dissolved in water toprecipitate the salts with impurities from the oil, and (vii) analysisof the oil extracted by gas liquid chromatography.
 4. The process asclaimed in claim 3 wherein the seeds of Momordica charantia L., aresplit, washed thoroughly with water 2–3 times to render the seedssubstantially free from impurities and dried under vacuum before saidgrinding.
 5. The process as claimed in claim 3 wherein the non-polarsolvent comprises a mixture of acetone with an aromatic or aliphatichydrocarbon selected from the group consisting of benzene, hexane,petroleum ether and ethyl ether.
 6. The process as claimed in claim 5wherein the ratio of the aliphatic or aromatic hydrocarbon in thenon-polar solvent mixture is 2:1.
 7. A method of treating a disease orcondition in a patient body, comprising applying the oil of claim 1 or acomposition comprising the oil of claim 1, on an affected area of thepatient body for a period of about six to twenty weeks, wherein thedisease or condition is selected from the group consisting of:inflammation, arthritis, vasculodilation and wounds.